P2Y1 receptor antagonists as novel antithrombotic agents

The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-06, Vol.18 (11), p.3338-3343
Hauptverfasser:	PFEFFERKORN, Jeffrey A, CHOI, Chulho, LEININGER, Michael T, GEYER, Andrew, SCHEFZICK, Sabine, ATHERTON, James, WINTERS, Thomas, KENNEDY, Robert, LIGUO CHI, PERRIN, Lisa A, LU, Gina, PING, Yun-Wen, MCCLANAHAN, Tom, SCHROEDER, Richard
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Diphosphate - pharmacology Administration, Oral Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Combinatorial Chemistry Techniques Drug Design Fibrinolytic Agents - chemical synthesis Fibrinolytic Agents - chemistry Fibrinolytic Agents - pharmacology Humans Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Platelet Aggregation - drug effects Purinergic P2 Receptor Antagonists Receptors, Purinergic P2Y1 Structure-Activity Relationship
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Zusammenfassung:	The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.04.028